WO1996003980A1 - Compositions effervescentes ameliorees - Google Patents
Compositions effervescentes ameliorees Download PDFInfo
- Publication number
- WO1996003980A1 WO1996003980A1 PCT/US1995/009540 US9509540W WO9603980A1 WO 1996003980 A1 WO1996003980 A1 WO 1996003980A1 US 9509540 W US9509540 W US 9509540W WO 9603980 A1 WO9603980 A1 WO 9603980A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- composition
- acid
- bicarbonate
- tablet
- weight
- Prior art date
Links
- 239000003826 tablet Substances 0.000 claims abstract description 18
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims abstract description 14
- 239000000796 flavoring agent Substances 0.000 claims abstract description 12
- 235000019634 flavors Nutrition 0.000 claims abstract description 12
- 239000002253 acid Substances 0.000 claims abstract description 11
- 235000003599 food sweetener Nutrition 0.000 claims abstract description 9
- 239000003765 sweetening agent Substances 0.000 claims abstract description 9
- 239000007938 effervescent tablet Substances 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims description 21
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 7
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 7
- 239000002245 particle Substances 0.000 claims description 6
- -1 alkali metal bicarbonate Chemical class 0.000 claims description 5
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 4
- 229910052783 alkali metal Inorganic materials 0.000 claims description 4
- 150000007524 organic acids Chemical class 0.000 claims description 4
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 2
- 235000019204 saccharin Nutrition 0.000 claims description 2
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims description 2
- 229940081974 saccharin Drugs 0.000 claims description 2
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 claims description 2
- 239000003381 stabilizer Substances 0.000 claims description 2
- 235000000346 sugar Nutrition 0.000 claims description 2
- 229960001295 tocopherol Drugs 0.000 claims description 2
- 229930003799 tocopherol Natural products 0.000 claims description 2
- 235000010384 tocopherol Nutrition 0.000 claims description 2
- 239000011732 tocopherol Substances 0.000 claims description 2
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims description 2
- 159000000000 sodium salts Chemical class 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 5
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 4
- 108010011485 Aspartame Proteins 0.000 description 3
- 239000000605 aspartame Substances 0.000 description 3
- 235000010357 aspartame Nutrition 0.000 description 3
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 3
- 229960003438 aspartame Drugs 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- CDBYLPFSWZWCQE-UHFFFAOYSA-L sodium carbonate Substances [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 3
- 150000001340 alkali metals Chemical class 0.000 description 2
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 description 2
- BSYNRYMUTXBXSQ-FOQJRBATSA-N 59096-14-9 Chemical compound CC(=O)OC1=CC=CC=C1[14C](O)=O BSYNRYMUTXBXSQ-FOQJRBATSA-N 0.000 description 1
- 150000005323 carbonate salts Chemical class 0.000 description 1
- 235000015872 dietary supplement Nutrition 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 235000019223 lemon-lime Nutrition 0.000 description 1
- 238000005461 lubrication Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000820 nonprescription drug Substances 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 235000011044 succinic acid Nutrition 0.000 description 1
- 150000003444 succinic acids Chemical class 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
Definitions
- Effervescent tablets containing medicinal or nutritional supplements are marketed worldwide as over-the-counter products. These tablets are added to water and dissolved with a characteristic effervescence, prior to ingestion. Although these formulations have the advantage of delivering medication in solution, they have the additional problem of requiring a high degree of flavoring to mask the taste of the incorporated medications or supplements. In addition, because of the high reactivity of the effervescent components the tablet is prone to stability problems and can also be very difficult to compress into a suitably hard tablet for packaging and sale. This invention provides a formulation which solves the latter problem.
- the preferred particle size of the acetylsalicylic acid is such that not more than 5% passes through a 40 mesh screen and not more than 20% passes through a 100 mesh screen, ie a normal distribution of particles between about 100 and 450 microns.
- Flavors are an important component of effervescent formulations. It has been found that high intensity flavors, containing tocopherol as a stabilizing agent provide better and more prolonged flavor stability in the composition of the invention. Such flavors are available from Firmenich Incorporated, Princeton, NJ. Preferably such flavors are incorporated at levels between 0.156 to about 0.5% of the tablet weight.
- Sweeteners are generally used in effervescent formulations. The preferred range for a sweetener in this composition is from about 0.4 lo 1.0 percent of the tablet weight. Any sweetener which imparts the necessary flavor may be used. Among the suggested sweeteners are sugar, aspartame and saccharin. Aspartame is a preferred sweetener.
- composition of the invention is further illustrated by the following example.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
Abstract
L'invention concerne un comprimé effervescent amélioré. Ce comprimé contient de l'acide acétylsalicylique, un rapport critique bicarbonate-acide, des substances aromatiques et édulcorantes, des adjuvants et, éventuellement, d'autres substances médicamenteuses. La stabilité et la dureté dudit comprimé ont été améliorées et il peut se préparer sous une forme compacte, afin d'obtenir un comprimé effervescent relativement petit en poids et en diamètre.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU31524/95A AU3152495A (en) | 1994-07-29 | 1995-07-28 | Improved effervescent delivery system |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28305794A | 1994-07-29 | 1994-07-29 | |
| US08/283,057 | 1994-07-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1996003980A1 true WO1996003980A1 (fr) | 1996-02-15 |
Family
ID=23084300
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1995/009540 WO1996003980A1 (fr) | 1994-07-29 | 1995-07-28 | Compositions effervescentes ameliorees |
Country Status (2)
| Country | Link |
|---|---|
| AU (1) | AU3152495A (fr) |
| WO (1) | WO1996003980A1 (fr) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2189639A1 (es) * | 2001-05-22 | 2003-07-01 | Cordon Jesus Angel Hernandez | Composicion acuosa que contiene acido acetilsalicilico |
| WO2023182904A1 (fr) * | 2022-03-21 | 2023-09-28 | Акционерное Общество "Производственная Фармацевтическая Компания Обновление" | Préparation médicamenteuse en poudre pour la préparation d'une solution, et procédé de production |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2211485A (en) * | 1940-08-13 | Effervescent acetyl salicylic acid |
-
1995
- 1995-07-28 AU AU31524/95A patent/AU3152495A/en not_active Abandoned
- 1995-07-28 WO PCT/US1995/009540 patent/WO1996003980A1/fr active Application Filing
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2211485A (en) * | 1940-08-13 | Effervescent acetyl salicylic acid |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2189639A1 (es) * | 2001-05-22 | 2003-07-01 | Cordon Jesus Angel Hernandez | Composicion acuosa que contiene acido acetilsalicilico |
| WO2023182904A1 (fr) * | 2022-03-21 | 2023-09-28 | Акционерное Общество "Производственная Фармацевтическая Компания Обновление" | Préparation médicamenteuse en poudre pour la préparation d'une solution, et procédé de production |
Also Published As
| Publication number | Publication date |
|---|---|
| AU3152495A (en) | 1996-03-04 |
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